Biochem/physiol Actions

Target K_i: 370 nM against rat brain CaM kinase II

Reversible: yes

Product competes with ATP.

Primary Targetcam kinase 2

Cell permeable: yes

General description

Cell-permeable, reversible, and competitive inhibitor of rat brain Ca⁺²/calmodulin-dependent protein kinase II (K_i = 370 nM). KN-93 selectively binds to the Calmodulin (CaM) binding site of the enzyme and prevents the association of CaM with CaM Kinase II. Selectively binds to the CaM binding site of the enzyme and prevents the association of CaM with CaMKII. Has no significant effect on protein kinase A activity. Induces G₁ cell cycle arrest and apoptosis in NIH 3T3 cells.

A cell-permeable, reversible and competitive inhibitor of rat brain CaM kinase II (K_i = 370 nM). Selectively binds to the CaM binding site of the enzyme and prevents the association of CaM with CaMKII. Has no significant effects on protein kinase A activity. Induces G₁ cell cycle arrest and apoptosis in NIH/3T3 cells. A 5 mM (1 mg/399 µl) solution of KN-93 (Cat. No. 422712) in DMSO is also available.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Fan, G.H., et al. 1999. Mol. Pharmacol.56, 39.Tombes, R.M., et al. 1995. Cell Growth Differ.6, 1063.Mamiya, N., et al. 1993. Biochem. Biophys. Res. Commun. 195, 608.Nicki, I., et al. 1993. Biochem. Biophys. Res. Commun.191, 255.Sumi, M., et al. 1991. Biochem. Biophys. Res. Commun.181, 968.Tokumitsu, H., et al. 1990. J. Biol. Chem.265, 4315.

Packaging

1, 5 mg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Warning

Toxicity: Irritant (B)